Related Experiment Video
Updated: May 10, 2026
Gene Regulation and Targeted Therapy in Gastric Cancer Peritoneal Metastasis: Radiological Findings from Dual Energy CT and PET/CT
Published on: January 22, 2018
Preclinical Assessment of a SuFEx-Modified, CAIX-Targeted PET Probe [68Ga]Ga-SF-DPI-4452 for Imaging Clear Cell Renal
You Cheng1,2, Yuhao Huang1, Yijin Zou1
1Department of Nuclear Medicine, Nanfang Hospital, Southern Medical University, Guangzhou North Road, Guangzhou, Guangdong 510515, China.
Abstract:
Carbonic anhydrase IX (CAIX) is an important target for imaging clear cell renal cell carcinoma (ccRCC), but existing probes show high gastrointestinal uptake. Here, a sulfur(VI) fluoride exchange (SuFEx)-modified PET probe, [68Ga]Ga-SF-DPI-4452, was developed to improve biodistribution. In vitro studies showed slightly lower CAIX affinity than [68Ga]Ga-DPI-4452 (IC50:7.53 vs 4.60 nM) but higher internalization (23% vs 7%). In OS-RC-2 tumor-bearing mice, both tracers displayed specific and high tumor uptake at 1 h postinjection ([68Ga]Ga-SF-DPI-4452:10.68 ± 2.25%ID/g vs [68Ga]Ga-DPI-4452:9.83 ± 5.86%ID/g, P > 0.05). Notably, [68Ga]Ga-SF-DPI-4452 significantly reduced gastrointestinal uptake, resulting in markedly improved tumor-to-background contrast (e.g., tumor-to-stomach ratio: 32.69 ± 15.51 vs 1.21 ± 0.34, P < 0.05). Biodistribution studies in mice and PET/CT imaging in cynomolgus monkeys further confirmed reduced gastrointestinal accumulation. Overall, SuFEx modification preserves tumor targeting while minimizing off-target uptake, supporting its potential for CAIX-targeted imaging and radionuclide therapy.
